EA200200990A1 - PHOSPHATIDYLINOSITOL-3-KINASE INHIBITORS DELTA HUMAN DELTA - Google Patents
PHOSPHATIDYLINOSITOL-3-KINASE INHIBITORS DELTA HUMAN DELTAInfo
- Publication number
- EA200200990A1 EA200200990A1 EA200200990A EA200200990A EA200200990A1 EA 200200990 A1 EA200200990 A1 EA 200200990A1 EA 200200990 A EA200200990 A EA 200200990A EA 200200990 A EA200200990 A EA 200200990A EA 200200990 A1 EA200200990 A1 EA 200200990A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pi3kδ
- methods
- inhibiting
- activity
- delta
- Prior art date
Links
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 1
- 238000000034 method Methods 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 4
- 230000002401 inhibitory effect Effects 0.000 abstract 4
- 102000038030 PI3Ks Human genes 0.000 abstract 2
- 108091007960 PI3Ks Proteins 0.000 abstract 2
- 102000001708 Protein Isoforms Human genes 0.000 abstract 2
- 108010029485 Protein Isoforms Proteins 0.000 abstract 2
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 210000000265 leukocyte Anatomy 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/28—Oxygen atom
- C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/36—Sulfur atom
- C07D473/38—Sulfur atom attached in position 6
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/40—Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
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- Dermatology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
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Abstract
Раскрыты способы ингибирования активности изоформы фосфатидилинозитол-3-киназы дельта (PI3Kδ) и способы лечения заболеваний, таких как нарушения иммунитета или воспаление, в которых PI3Kδ играет роль в функции лейкоцитов. Преимущественно способы используют активные агенты, которые селективно ингибируют PI3Kδ, в то время как незначительно ингибируют активность других изоформ PI3K. Обеспечены соединения, которые ингибируют активность PI3Kδ, включая соединения, которые селективно ингибируют активность PI3Kδ. Обеспечены способы использования соединений, ингибирующих PI3Kδ, для ингибирования роста или пролиферации раковых клеток. Соответственно, изобретение обеспечивает способы применения соединений, ингибирующих PI3Kδ, для ингибирования процессов, опосредованных PI3Kδ, in vitro и in vivo.Отчет о международном поиске был опубликован 2002.03.21.Disclosed are methods for inhibiting the activity of the phosphatidylinositol-3-kinase delta (PI3Kδ) isoform and methods for treating diseases, such as immune disorders or inflammation, in which PI3Kδ plays a role in the function of white blood cells. Advantageously, the methods use active agents that selectively inhibit PI3Kδ, while slightly inhibit the activity of other PI3K isoforms. Compounds that inhibit PI3Kδ activity are provided, including compounds that selectively inhibit PI3Kδ activity. Provided methods of using compounds that inhibit PI3Kδ for inhibiting the growth or proliferation of cancer cells. Accordingly, the invention provides methods for using compounds inhibiting PI3Kδ for inhibiting PI3Kδ-mediated processes in vitro and in vivo. An international search report was published 2002.03.21.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US19965500P | 2000-04-25 | 2000-04-25 | |
US23805700P | 2000-10-05 | 2000-10-05 | |
PCT/US2001/013315 WO2001081346A2 (en) | 2000-04-25 | 2001-04-24 | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200200990A1 true EA200200990A1 (en) | 2003-06-26 |
EA008241B1 EA008241B1 (en) | 2007-04-27 |
Family
ID=26894992
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200200990A EA008241B1 (en) | 2000-04-25 | 2001-04-24 | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
Country Status (27)
Country | Link |
---|---|
US (2) | US6518277B1 (en) |
EP (3) | EP3029041B1 (en) |
JP (1) | JP4642309B2 (en) |
KR (1) | KR100785363B1 (en) |
CN (1) | CN1440408B (en) |
AT (1) | ATE502941T1 (en) |
AU (2) | AU5566701A (en) |
BR (1) | BRPI0110371B8 (en) |
CA (1) | CA2406278C (en) |
CY (1) | CY1117672T1 (en) |
DE (1) | DE60144277D1 (en) |
DK (3) | DK1278748T3 (en) |
EA (1) | EA008241B1 (en) |
ES (3) | ES2527754T3 (en) |
GE (1) | GEP20084317B (en) |
HK (1) | HK1053308A1 (en) |
HR (1) | HRP20020838A2 (en) |
HU (1) | HU230554B1 (en) |
IL (3) | IL152275A0 (en) |
IS (1) | IS2822B (en) |
MX (1) | MXPA02010618A (en) |
NO (2) | NO329136B1 (en) |
NZ (1) | NZ522076A (en) |
PT (3) | PT1939203E (en) |
RS (1) | RS51458B (en) |
SI (2) | SI2223922T1 (en) |
WO (1) | WO2001081346A2 (en) |
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US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
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US6608053B2 (en) * | 2000-04-27 | 2003-08-19 | Yamanouchi Pharmaceutical Co., Ltd. | Fused heteroaryl derivatives |
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US7829084B2 (en) * | 2001-01-17 | 2010-11-09 | Trubion Pharmaceuticals, Inc. | Binding constructs and methods for use thereof |
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EP1442132A2 (en) * | 2001-10-26 | 2004-08-04 | Novartis AG | Methods for the treatment of osteoarthritis and compositions thereof |
EP1444209A4 (en) * | 2001-11-07 | 2005-02-16 | Merck & Co Inc | Mitotic kinesin inhibitors |
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TWI314928B (en) | 2002-02-28 | 2009-09-21 | Novartis A | 5-phenylthiazole derivatives and use as pi3 kinase inhibitors |
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EP1513820A4 (en) * | 2002-05-23 | 2006-09-13 | Cytokinetics Inc | Compounds, compositions, and methods |
JP2005538062A (en) * | 2002-06-14 | 2005-12-15 | サイトキネティクス・インコーポレーテッド | Compounds, compositions and methods |
EP1542703A4 (en) * | 2002-07-10 | 2007-11-07 | Massachusetts Inst Technology | Solid-phase and solution-phase synthesis of glycosylphosphatidylinositol glycans |
JP2006501201A (en) * | 2002-07-23 | 2006-01-12 | サイトキネティクス・インコーポレーテッド | Compounds, compositions and methods |
JP2005536553A (en) * | 2002-08-21 | 2005-12-02 | サイトキネティクス・インコーポレーテッド | Compounds, compositions and methods |
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WO2004056820A1 (en) * | 2002-12-20 | 2004-07-08 | Warner-Lambert Company Llc | Benzoxazines and derivatives thereof as inhibitors of pi3ks |
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